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THE PHARMA REVIEW (NOVEMBER 2009)

Novel Nanostructured Lipidic Drug Delivery Systems

Bhupinder Singh, Shantanu Bandyopadhyay, Rishi Kapil, O.P. Katare

Abstracts: We are amidst a nano-era. Nanotechnology, for that matter, has emerged as a contemporary discipline with novel applications in drug delivery research as well. Literally, the Greek word, “nano” signifies “a billionth” (i.e., of a meter). It verily implies tiny particles, even much smaller than a living cell. Nano-sized particles range form nano-liposomes, to dendrimers, to self nano-emulsifying systems, to quantum dots, to carbon-based nanoparticles like nano-tubes and nano-fibers. Lately, the global pharma world has witnessed tremendous headway in introducing innovative nanotechnologies, exploring their applications in temporal and spatial drug delivery, addressing their toxicity concerns and resolving key federal issues.
 
Nanostructured or nanoparticulate drug delivery systems, accordingly, are gaining increased recognition worldwide. There are tangible applications of nanosystems in the domains of drug delivery or gene delivery, like delivering small particles in the tumors, across the blood-brain barrier and other impregnable sites through diverse routes of drug administration.
 
Lipid-based nanoparticulate matrices in the form of “lipid pellets”, known from the textbooks since decades, are available till date as products like Mucosolvan retard (Boehringer Ingelheim). Subsequent to these first-generation lipid pellets, the second-generation “lipid nanopellets” were developed for oral administration in the mid-eighties. This system, however, could not be further developed, primarily due to non-existential patent protection in many countries then. At the beginning of the nineties, the third generation products were evolved as “solid lipid nanoparticles” (SLNs). These submicron size range (50–1000 nm) particles, made up of biocompatible and biodegradable materials, and capable of incorporating lipophilic and hydrophilic drugs, have withstood the test of time till date. The general structure of SLNs is shown in Fig. 1.
 
Common constituents employed during the formulation of SLNs include the lipids (i.e., matrix materials), emulsifiers, co-emulsifiers and water. Charge modifiers and stealthing agents that improve long circulation time and targeting ability, are also used to meet the requirements of stability and targeting. SLNs combine the advantages of different colloidal carriers. For instance, these are physiologically acceptable like emulsions and liposomes, capable of yielding controlled release characteristics of drug from lipid matrices like polymeric nanoparticles. SLNs have high potential to be exploited as delivery system on industrial scale. However, there are certain shortcomings associated with the SLN system:

  

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